AP2000001944A0 - Nonnucleoside inhibitors of reverse transcriptase for the treatment of HIV-infection. - Google Patents

Nonnucleoside inhibitors of reverse transcriptase for the treatment of HIV-infection.

Info

Publication number
AP2000001944A0
AP2000001944A0 APAP/P/2000/001944A AP2000001944A AP2000001944A0 AP 2000001944 A0 AP2000001944 A0 AP 2000001944A0 AP 2000001944 A AP2000001944 A AP 2000001944A AP 2000001944 A0 AP2000001944 A0 AP 2000001944A0
Authority
AP
ARIPO
Prior art keywords
hiv
reverse transcriptase
composite
nni
novel compounds
Prior art date
Application number
APAP/P/2000/001944A
Inventor
Rakesh Vig
Chen Mao
Fatih M Uckun
Original Assignee
Parker Hughes Inst
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Parker Hughes Inst filed Critical Parker Hughes Inst
Publication of AP2000001944A0 publication Critical patent/AP2000001944A0/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine

Abstract

Novel compounds that are potent inhibitors of hiv reverse transcriptase (rt)are described in the invention. These novel compounds also inhibit replication of a retrovirus, such as human immunodeficiency virus-1 (hiv-1). The novel compounds of the invention include analogs and derivatives of phenethylthiazolythiourea (pett), of dihydroalkoxybenzy-loxopyrimidine (dabo), and of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (hept). The invention additionally provides a composite hiv reverse-transcriptase (rt)nonnucleoside inhibitor (nni)binding pocket constructed from a composite of multiple nni-rt complexes. The composite rt-nni binding pocket provides a unique and useful tool for designing and identifying novel, potent inhibitors of reverse transcriptase.
APAP/P/2000/001944A 1998-03-17 1999-03-16 Nonnucleoside inhibitors of reverse transcriptase for the treatment of HIV-infection. AP2000001944A0 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US09/040,538 US5998411A (en) 1998-03-17 1998-03-17 Heterocyclic nonnucleoside inhibitors of reverse transcriptase
PCT/US1999/005602 WO1999047501A2 (en) 1998-03-17 1999-03-16 Nonnucleoside inhibitors of reverse transcriptase for the treatment of hiv-infection

Publications (1)

Publication Number Publication Date
AP2000001944A0 true AP2000001944A0 (en) 2000-12-31

Family

ID=21911533

Family Applications (1)

Application Number Title Priority Date Filing Date
APAP/P/2000/001944A AP2000001944A0 (en) 1998-03-17 1999-03-16 Nonnucleoside inhibitors of reverse transcriptase for the treatment of HIV-infection.

Country Status (11)

Country Link
US (8) US5998411A (en)
EP (2) EP1064263B1 (en)
JP (1) JP2002506854A (en)
CN (1) CN1301254A (en)
AP (1) AP2000001944A0 (en)
AT (1) ATE312079T1 (en)
AU (1) AU752010B2 (en)
CA (1) CA2323418A1 (en)
DE (1) DE69928779T2 (en)
EA (1) EA200000958A1 (en)
WO (1) WO1999047501A2 (en)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5998411A (en) 1998-03-17 1999-12-07 Hughes Institute Heterocyclic nonnucleoside inhibitors of reverse transcriptase
IT1305313B1 (en) * 1998-07-17 2001-05-04 Colla Paolo 3,4 - DIHYDRO- 6- BENZYL-4-OXOPYRIMIDINE REPLACED AND RELATED PROCESS OF PRODUCTION AND USE IN THE THERAPY OF HIV-1 INFECTIONS.
US6136335A (en) * 1998-12-31 2000-10-24 Hughes Institute Phenethyl-5-bromopyridylthiourea (PBT) and dihydroalkoxybenzyloxopyrimidine (DABO) derivatives exhibiting spermicidal activity
US7186736B1 (en) 1999-03-20 2007-03-06 Parker Hughes Institute NNI for treatment of multi-drug resistant HIV
US6207688B1 (en) * 1999-06-23 2001-03-27 Parker Hughes Institute Phenethyl-thiourea compounds and use
US6545152B1 (en) * 2000-07-18 2003-04-08 Parker Hughes Institute R-isomers of nonnucleoside inhibitors
US6960606B2 (en) * 2000-10-19 2005-11-01 Parker Hughes Institute Adamantyl Thiazole Thioureas
US6689793B2 (en) * 2000-12-06 2004-02-10 Parker Hughes Institute Piperidinylethyl-, phenoxyethyl-, and β-fluorophenethyl-substituted thiourea compounds with potent anti-HIV activity
SE0100733D0 (en) 2001-03-05 2001-03-05 Medivir Ab Non-nucleoside reverse transcriptase inhibitors
US7642277B2 (en) * 2002-12-04 2010-01-05 Boehringer Ingelheim International Gmbh Non-nucleoside reverse transcriptase inhibitors
TW200600492A (en) 2004-05-18 2006-01-01 Achillion Pharmaceuticals Inc Substituted aryl acylthioureas and related compounds; inhibitors of viral replication
US7892618B2 (en) 2005-03-21 2011-02-22 Sony Corporation Deterring theft of optical media
US7702625B2 (en) * 2006-03-03 2010-04-20 International Business Machines Corporation Building a unified query that spans heterogeneous environments
KR20090040449A (en) * 2006-07-24 2009-04-24 길리애드 사이언시즈, 인코포레이티드 Novel hiv reverse transcriptase inhibitors
MX2009013804A (en) * 2007-06-29 2010-02-03 Korea Res Inst Chem Tech Novel hiv reverse transcriptase inhibitors.
WO2009005693A1 (en) * 2007-06-29 2009-01-08 Gilead Sciences, Inc. Novel hiv reverse transcriptase inhibitors
KR20100092960A (en) * 2007-12-21 2010-08-23 한국화학연구원 Processes for preparing hiv reverse transcriptase inhibitors
CN103288719A (en) * 2012-03-05 2013-09-11 苏州欧凯医药技术有限公司 Synthesis of non-nucleoside HIV (human immunodeficiency virus) inhibitor pyridone lead
US9471130B2 (en) * 2013-10-25 2016-10-18 Advanced Micro Devices, Inc. Configuring idle states for entities in a computing device based on predictions of durations of idle periods
CN107301327A (en) * 2017-05-17 2017-10-27 华南理工大学 A kind of method that use computer simulation metal complex interacts with DNA
CN108010101A (en) * 2017-12-18 2018-05-08 重庆大学 A kind of method for drawing molecule fragment 2D perspective views

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5112835A (en) * 1988-03-31 1992-05-12 Mitsubishi Kasei Corporation 6-substituted acyclopyrimidine nucleoside derivatives and antiviral agents containing the same as active ingredient thereof
US5686428A (en) * 1989-04-07 1997-11-11 Aktiebolaget Astra Pharmaceutical composition
HU205917B (en) * 1989-09-29 1992-07-28 Mitsubishi Chem Ind Process for producing 6-substituted pyrimidine derivatives and antiviral pharmaceutical compositions containing them as active components
EP0449726B1 (en) * 1990-03-29 1997-06-11 Mitsubishi Chemical Corporation Pyrimidine nucleoside derivative and antiviral agent containing the derivative as active ingredient
US5503978A (en) * 1990-06-11 1996-04-02 University Research Corporation Method for identification of high affinity DNA ligands of HIV-1 reverse transcriptase
US5593993A (en) * 1991-08-02 1997-01-14 Medivir Ab Method for inhibition of HIV related viruses
IL102548A (en) 1991-08-02 1998-08-16 Medivir Ab Thiourea derivatives for use in the preparation of medicaments for the inhibition of hiv and the treatment of aids and some such novel compounds
JPH0725770A (en) 1993-07-09 1995-01-27 Mitsubishi Chem Corp Percutaneously absorbefacient antiviral agent
KR100326621B1 (en) 1993-08-24 2002-07-27 메디비르 아베 Compounds and methods for inhibiting human immunodeficiency virus and related viruses
US5998411A (en) 1998-03-17 1999-12-07 Hughes Institute Heterocyclic nonnucleoside inhibitors of reverse transcriptase

Also Published As

Publication number Publication date
JP2002506854A (en) 2002-03-05
EP1064263A2 (en) 2001-01-03
AU3186499A (en) 1999-10-11
WO1999047501A3 (en) 1999-12-02
US6300351B1 (en) 2001-10-09
US6925388B1 (en) 2005-08-02
WO1999047501A2 (en) 1999-09-23
CA2323418A1 (en) 1999-09-23
EA200000958A1 (en) 2001-06-25
US6380190B1 (en) 2002-04-30
US5998411A (en) 1999-12-07
DE69928779D1 (en) 2006-01-12
US6156759A (en) 2000-12-05
US20050153995A1 (en) 2005-07-14
CN1301254A (en) 2001-06-27
US6124307A (en) 2000-09-26
EP1528057A1 (en) 2005-05-04
DE69928779T2 (en) 2006-11-02
AU752010B2 (en) 2002-09-05
ATE312079T1 (en) 2005-12-15
EP1064263B1 (en) 2005-12-07
US6180654B1 (en) 2001-01-30

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